PFK15

Dangerous Goods

CAS number：4382-63-2 molecular formula：C17H12N2O

overview

Specs

numbering system

physicochemical properties

Safety information

Production methods and uses

MSDS

overview

compound introduction

PFK-015是PFKFB3抑制剂，对重组PFKFB3的IC50为110 nM，能抑制肿瘤细胞内PFKFB3活性，IC50为20 nM。 PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM. IC50 value: 110 nM (recombinant PFKFB3)[1] Target: PFKFB3 PFK-015 possesses compelling in vitro properties, has satisfactory PK properties in rodents, and suppresses tumor glucose metabolism and growth in an aggressive mouse model of non-small cell lung cancer. PFK-015 is not a Pgp substrate as determined by transport and cell permeability assays in Caco-2 and MDCK-MDR1 (Papp A-B / B-A results 1.8 / 4 and 5 / 5 10–6 cm/s). PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines. PFK-015 suppresses glucose uptake in cancer cells. Rodent PK studies following IV dosing at 5 mg/kg resulted in a profile with a satisfactory half-life (5.1 hours), exposure (AUCinf 1804 ng.h/ml), tissue distribution (Vd 20.5 L/kg) and reasonable clearance (46.2 mL/min/kg). Also, pre-clinical efficacy studies of C57Bl/6 mice bearing Lewis Lung Carcinoma (LLC) xenografts demonstrated 80% tumor growth inhibition relative to vehicle control. Finally, micro-PET studies performed on mice bearing LLC tumors showed a significant inhibition of tumor 2-[18F]-fluoro-2-deoxy-glucose uptake. These results support further development of PFK-015 as a novel anti-cancer agent.

Specs

Chinese alias	-
English alias	PFK015 \| PFK-015 \| 1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one \| PFK 015 \| SCHEMBL2702934 \| HY-12204 \| EN300-22345725 \| PFK 15 \| HSDB 3055 \| AKOS025287166 \| NCGC00386328-09 \| C75180 \| EX-A4218 \| 1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one \| SW21
CAS number	4382-63-2	molecular formula	C17H12N2O
molecular weight	260.29 g/mol	Exact mass	-
PSA	42.900 Å²	logp	2.9

numbering system

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physicochemical properties

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Safety information

pictogram：

GHS07

Signal word：

Warning

Hazard Statement：

H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激

Statement of Preventive Measures：

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P304+P340: 如误吸入：将人转移

WGK Germany：